GSK3368715 (Synonyms: EPZ019997)

Name: GSK3368715
Brand: MedChemExpress
SKU: HY-128717
Rating: 5.0 (18 reviews)

Cat. No.: HY-128717 Purity: 99.41%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

GSK3368715 (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC₅₀=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No. : 1629013-22-4

사이즈	재고	수량
Oil + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Oil
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	견적 받기
200 mg	견적 받기

or 대량구매 문의

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 18 publication(s) in Google Scholar

Other Forms of GSK3368715:

18 Publications Citing Use of MCE GSK3368715

Cell Proliferation/Viability Assay

In Vivo Efficacy Study

: GSK3368715 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2024 Dec;20(12):1566-1576. [Abstract]; Immunoblot analysis and quantification of GSK3β-SNAP in MrTAC-treated HEK293T cells (10 μM; 3 h) in the presence of GSK368715 (10 μM).

: GSK3368715 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 23;14(1):1011. [Abstract]; PRMT1 inhibitor GSK3368715 (2 μM) markedly reduced the growth of HCC cells in vitro.

: GSK3368715 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 23;14(1):1011. [Abstract]; Images, weight, and volume of Huh7 tumor xenografts from BALB/c nude mice fed with a -SG diet and treated with or without GSK3368715 (100 mg/kg; p.o.; every other day).

: GSK3368715 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 23;14(1):1011. [Abstract]; GSK3368715 (2 μM; 6 h) blocked the binding of nonmethylated peptide with PRMT1 in Huh7 and PLC/PRF/5 cells.

: GSK3368715 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 23;14(1):1011. [Abstract]; Endogenous PHGDH was immunoprecipitated in Huh7 and PLC/PRF/5 cells treated with or without the PRMT1 inhibitor GSK3368715 (2 μM).

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target

PRMT1

PRMT4

PRMT3

PRMT6

PRMT8

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	38.25 μM Compound: 6; GSK3368715	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth by CCK-8 assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth by CCK-8 assay	[PMID: 38460270]

In Vitro

GSK3368715 (EPZ019997) shows 50% or more growth inhibition relative to DMSO-treated cells in the majority of 249 cancer cell lines, representing 12 tumor types^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GSK3368715 (EPZ019997) significantly effects on the growth of BxPC3 xenografts at all doses tested, reducing tumor growth by 78% and 97% in the 150- and 300-mg/kg dose groups, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

분자량

366.54

화학식

C₂₀H₃₈N₄O₂

CAS No.

1629013-22-4

Appearance

Oil

Color

Colorless to light yellow

SMILES

CNCCN(CC1=CNN=C1C2CCC(COCC)(COCC)CC2)C

선적

Room temperature in continental US; may vary elsewhere.

보관

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

용액&용해도

In Vitro:

DMSO : 5 mg/mL (13.64 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7282 mL	13.6411 mL	27.2822 mL
5 mM	0.5456 mL	2.7282 mL	5.4564 mL
10 mM	0.2728 mL	1.3641 mL	2.7282 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

몰농도 계산기
농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.83 mg/mL (2.26 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.83 mg/mL (2.26 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.83 mg/mL (2.26 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

순도&문서

Purity: 99.41%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (254 KB) HNMR (309 KB) RP-HPLC (255 KB) MS (69 KB)

Handling Instructions (2659 KB)

References

[1]. Fedoriw A, et al. Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss. Cancer Cell. 2019 Jul 8;36(1):100-114.e25. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.7282 mL	13.6411 mL	27.2822 mL	68.2054 mL
	5 mM	0.5456 mL	2.7282 mL	5.4564 mL	13.6411 mL
	10 mM	0.2728 mL	1.3641 mL	2.7282 mL	6.8205 mL

GSK3368715 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK33687151629013-22-4EPZ019997GSK 3368715GSK-3368715EPZ 019997EPZ-019997Histone MethyltransferaseInhibitorinhibitorinhibit

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GSK3368715 (Synonyms: EPZ019997)

고객리뷰

Other Forms of GSK3368715:

GSK3368715 Related Antibodies

18 Publications Citing Use of MCE GSK3368715

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

Biological Activity

순도&문서

References

고객리뷰

GSK3368715 Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

GSK3368715 Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report